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867063-97-6

867063-97-6 Structure

867063-97-6 Structure
IdentificationBack Directory
[Name]

Atiratecan
[CAS]

867063-97-6
[Synonyms]

TP300
Atiratecan
CWJSAEZZZABNRI-HKBQPEDESA-N
Glycine, glycyl-N-methyl-, (9S)-9-ethyl-9,10,13,15-tetrahydro-10,13-dioxo-1-pentyl-1H,12H-pyrano[3'',4'':6',7']indolizino[2',1':5,6]pyrido[4,3,2-de]quinazolin-9-yl ester
[Molecular Formula]

C31H34N6O6
[MDL Number]

MFCD19443718
[MOL File]

867063-97-6.mol
[Molecular Weight]

586.64
Chemical PropertiesBack Directory
[Boiling point ]

936.0±75.0 °C(Predicted)
[density ]

1.45±0.1 g/cm3(Predicted)
[pka]

8.09±0.10(Predicted)
Hazard InformationBack Directory
[Uses]

Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1].
[in vivo]

Atiratecan (TP300; 47 mg/kg; IV; once per week for 3 weeks) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP[1].
Atiratecan (24 mg/kg; IV; once per week for 6 weeks) in combination with capecitabine results in synergistic eVects in the HCT116 human colon cancer and NCI-N87 human gastric cancer xenograft models and an additive eVect in the WiDr human colon cancer xenograft model which is BCRP-positive and CPT-11-insensitive[1].
The eVective dose range of Atiratecan is between 0.30 and 47 mg/kg (MTD/ED50=157). The toxic dose is 63 mg/kg for Atiratecan[1].

Animal Model:Five-week-old male athymic nude mice (CAnN.CgFoxn1nu/CrlCrlj)[1]
Dosage:47 mg/kg (the maximum tolerated dose; MTD)
Administration:IV; once per week for 3 weeks
Result:Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP.
[References]

[1] Endo M, et al. A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancerresistance protein-expressing tumor xenografts. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71. DOI:10.1007/s00280-009-1042-5
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